Sigma Receptor
Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body. The endogenous ligand for these sites has not been identified, but steroid hormones (particularly progesterone), sphingolipid-derived amines and N,N-dimethyltryptamine can bind with fairly high affinity.
The sigma-1 receptor (σ1R) is an endoplasmic reticulum (ER)-resident chaperone protein that acts like an inter-organelle signaling modulator. It participates in many biological processes including nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer’s disease. The sigma-2 (σ2R) receptor is overexpressed in various human tumors. It has been validated as a biomarker for proliferating tumors.
Sigma Receptor Isoform Specific Products
All Product Categories
-
Sigma Receptor Inhibitors
(16)
View all products
-
Sigma Receptor Agonists
(54)
View all products
-
Sigma Receptor Antagonists
(60)
View all products
-
Sigma Receptor Activators
(10)
View all products
-
Sigma Receptor Modulators
(8)
View all products
-
Sigma Receptor Control
(1)
View all products
-
Sigma Receptor Ligands
(10)
View all products
-
Sigma Receptor Related Products (195)
Related Products (195)
-
Sigma Receptor Isoform Comparison
-
SW116 free base
0 ImagesCat. No.: HY-120421CAS No.: 1036759-00-8SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research.
-
N-Desmethyl xanomeline
0 ImagesCat. No.: HY-181425CAS No.: 131986-96-4N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline (HY-105182). N-Desmethyl xanomeline binds to muscarinic, serotonergic, histaminergic and dopaminergic receptors. N-Desmethyl xanomeline can be used for the research of schizophrenia.
-
Rimcazole dihydrochloride (Standard)
0 ImagesCat. No.: HY-108510RCAS No.: 75859-03-9Synonyms: BW 234U dihydrochloride (Standard)Rimcazole dihydrochloride (Standard) is the analytical standard of Rimcazole (dihydrochloride) (HY-108510). This product is intended for research and analytical applications. Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.
-
Sigma-2 Receptor ligand 2
0 ImagesCat. No.: HY-184175CAS No.: 1816276-88-6Sigma-2 Receptor ligand 2 is a fluorescence labeled sigma-2 ligand. Sigma-2 Receptor ligand 2 can be used as a fluorescent probe.
-
(±)-PPCC
0 ImagesCat. No.: HY-111081CAS No.: 932736-90-8(±)-PPCC is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.
-
KSCM-1
0 ImagesCat. No.: HY-118279CAS No.: 1415247-17-4KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors.
-
Blarcamesine hydrochloride (Standard)
0 ImagesCat. No.: HY-101864RCAS No.: 195615-84-0Synonyms: Anavex 2-73 (Standard)Blarcamesine hydrochloride (Standard) is the analytical standard of Blarcamesine hydrochloride (HY-101864). This product is intended for research and analytical applications. Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
-
BD-1063
0 ImagesCat. No.: HY-18101CAS No.: 150208-28-9BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.
-
BD-1047 dihydrobromide (Standard)
0 ImagesBD-1047 (dihydrobromide) (Standard) is the analytical standard of BD-1047 (dihydrobromide). This product is intended for research and analytical applications. BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.
-
Convolamine hydrochloride
0 ImagesCat. No.: HY-N15339ACAS No.: 5896-59-3Convolamine hydrochloride is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC50 value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease.
-
Blonanserin (Standard)
0 ImagesSynonyms: AD-5423 (Standard)Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
-
Opipramol-d4
0 ImagesCat. No.: HY-118901SCAS No.: 1215716-70-3Synonyms: Ensidon-d4; G-33040-d4Opipramol-d4 is the deuterium labeled Opipramol.
-
Zervimesine (Standard)
0 ImagesCat. No.: HY-111669RCAS No.: 1802632-22-9Synonyms: CT1812 (Standard); Sigma-2 receptor antagonist 1 (Standard)Zervimesine (Standard) is the analytical standard of Zervimesine (HY-111669). This product is intended for research and analytical applications. Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease.
-
4-IBP (Standard)
0 Images4-IBP (Standard) is the analytical standard of 4-IBP (HY-100155). This product is intended for research and analytical applications. 4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research.
-
Cinuperone
0 ImagesCat. No.: HY-W754019CAS No.: 82117-51-9Cinuperone is a multi-target competitive receptor ligand and σ receptor antagonist that acts on Dopamine D1, σ, Dopamine D1, and 5-HT2 receptors. Cinuperone shows significantly higher affinity for σ receptors than for Dopamine D1 receptors, and only exhibits moderate binding activity for dopamine D2 receptors. Cinuperone can be used in the research of central nervous system diseases.
-
Thiothixene
0 ImagesThiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
-
Blarcamesine (Standard)
0 ImagesBlarcamesine (Standard) is the analytical standard of Blarcamesine (HY-105296). This product is intended for research and analytical applications. Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
-
BMY-14802 hydrochloride (Standard)
0 ImagesCat. No.: HY-108509RCAS No.: 105565-55-7Synonyms: BMY-14802-1 (Standard); BMS 181100 hydrochloride (Standard)BMY-14802 hydrochloride (Standard) is the analytical standard of BMY-14802 (hydrochloride) (HY-108509). This product is intended for research and analytical applications. BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
-
Chlophedianol hydrochloride (Standard)
0 ImagesCat. No.: HY-A0161ARCAS No.: 511-13-7Synonyms: Clofedanol hydrochloride (Standard); Calmotusin hydrochloride (Standard); NSC 113595 hydrochloride (Standard)Chlophedianol (hydrochloride) (Standard) is the analytical standard of Chlophedianol (hydrochloride). This product is intended for research and analytical applications. Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs).
